APINACA (AKB48, ''N''-(1-adamantyl)-1-pentyl-1''H''-indazole-3-carboxamide) is a drug that acts as a reasonably potent
agonist
An agonist is a chemical that activates a receptor to produce a biological response. Receptors are cellular proteins whose activation causes the cell to modify what it is currently doing. In contrast, an antagonist blocks the action of the ago ...
for the
cannabinoid receptor
Cannabinoid receptors, located throughout the body, are part of the endocannabinoid system a class of cell membrane receptors in the G protein-coupled receptor superfamily. As is typical of G protein-coupled receptors, the cannabinoid recep ...
s, with a K
i of 304.5nM and an EC
50 of 585nM at
CB1. It had never previously been reported in the scientific or patent literature, and was first identified by laboratories in Japan in March 2012 as an ingredient in
synthetic cannabis
Synthetic cannabinoids are a class of designer drug molecules that bind to the same receptors to which cannabinoids ( THC, CBD and many others) in cannabis plants attach. These novel psychoactive substances should not be confused with syntheti ...
smoking blends, along with a related compound
APICA. Structurally, it closely resembles cannabinoid compounds from a University of Connecticut patent (WO 2003/035005), but with a simple pentyl chain on the indazole 1-position, and APINACA falls within the claims of this patent despite not being disclosed as an example.
Legality
APINACA was made illegal in Japan in 2012, and was banned as a
temporary class drug
A temporary class drug is a relatively new status for controlled drugs, which has been adopted in some jurisdictions, notably New Zealand and the United Kingdom, to attempt to bring newly synthesised designer drugs under legal control. The controll ...
in New Zealand from 13 July 2012.
APINACA has been banned in Latvia since 14 November 2013.
Since 2013, APINACA has been a Schedule I controlled substance in the United States.
It is also banned in Germany as an
Anlage II
Anlage may refer to:
* Allele, a specific version of a gene, as used by Gregor Mendel
* Anlage Süd, a headquarters facility of the German Third Reich in Strzyżów, Poland
* Primordium, the initial clustering of embryonic cells from which a body ...
controlled drug.
APINACA is listed in the Fifth Schedule of the Misuse of Drugs Act (MDA) and therefore illegal in Singapore as of May 2015.
As of October 2015 APINACA is a controlled substance in China.
APINACA is banned in the Czech Republic.
Detection
A forensic standard of APINACA is available, and the compound has been posted on the Forendex website of potential drugs of abuse.
See also
*
5F-AB-PINACA
5F-AB-PINACA is an indazole-based synthetic cannabinoid that is derived from a series of compounds originally developed by Pfizer in 2009 as an analgesic medication, and has been sold online as a designer drug.
5F-AB-PINACA has been reported t ...
*
5F-ADB
5F-ADB (also known as 5F-MDMB-PINACA) is an indazole-based synthetic cannabinoid from the indazole-3-carboxamide family, which has been used as an active ingredient in synthetic cannabis products and has been sold online as a designer drug. 5F- ...
*
5F-AMB
5F-AMB (also known as 5F-MMB-PINACA and 5F-AMB-PINACA) is an indazole-based synthetic cannabinoid from the indazole-3-carboxamide family, which has been used as an active ingredient in synthetic cannabis products. It was first identified in Jap ...
*
5F-APINACA
5F-APINACA (also known as 5F-AKB-48 or 5F-AKB48) is an indazole-based synthetic cannabinoid that has been sold online as a designer drug. Structurally it closely resembles cannabinoid compounds from patent WO 2003/035005 but with a 5-fluoropent ...
*
5F-CUMYL-PINACA
*
AB-CHFUPYCA
*
AB-CHMINACA
AB-CHMINACA is an indazole-based synthetic cannabinoid. It is a potent agonist of the CB1 receptor (''K''i = 0.78 nM) and CB2 receptor (''K''i = 0.45 nM) and fully substitutes for Δ9-THC in rat discrimination st ...
*
AB-FUBINACA
AB-FUBINACA is a drug that acts as a potent agonist for the cannabinoid receptors, with ''K''i values of 0.9 nM at CB1 and 23.2 nM at CB2 and EC50 values of 1.8 nM at CB1 and 3.2 nM at CB2. It was originally developed by P ...
*
AB-PINACA
AB-PINACA is a compound that was first identified as a component of synthetic cannabis products in Japan in 2012.
It was originally developed by Pfizer in 2009 as an analgesic medication.
AB-PINACA acts as a potent agonist for the CB1 recepto ...
*
ADAMANTYL-THPINACA
*
ADB-CHMINACA
*
ADB-FUBINACA
ADB-FUBINACA is a designer drug identified in synthetic cannabis blends in Japan in 2013. In 2018, it was the third-most common synthetic cannabinoid identified in drugs seized by the Drug Enforcement Administration.
The (''S'')-enantiomer of A ...
*
ADB-PINACA
ADB-PINACA is a cannabinoid designer drug that is an ingredient in some synthetic cannabis products. It is a potent agonist of the CB1 receptor and CB2 receptor with EC50 values of 0.52 nM and 0.88 nM respectively. Like MDMB-FUBINA ...
*
ADBICA
ADBICA (also known as ADB-PICA) is a designer drug identified in synthetic cannabis blends in Japan in 2013. ADBICA had not previously been reported in the scientific literature prior to its sale as a component of synthetic cannabis blends. ADBI ...
*
APICA
*
FUB-APINACA
*
MDMB-CHMICA
*
PX-3
PX-3 (also known as APP-CHMINACA) is an indazole-based synthetic cannabinoid. It is a potent agonist of the CB1 receptor with a binding affinity of ''K''i = 47.6 nM and was originally developed by Pfizer in 2009 as an analgesic
...
*
SDB-001
*
STS-135
STS-135 (ISS assembly flight ULF7) was the 135th and final mission of the American Space Shuttle program. It used the orbiter '' Atlantis'' and hardware originally processed for the STS-335 contingency mission, which was not flown. STS-135 l ...
*
Synthetic cannabinoid
Synthetic cannabinoids are a class of designer drug molecules that bind to the same receptors to which cannabinoids ( THC, CBD and many others) in cannabis plants attach. These novel psychoactive substances should not be confused with synth ...
*
Synthetic cannabis
Synthetic cannabinoids are a class of designer drug molecules that bind to the same receptors to which cannabinoids ( THC, CBD and many others) in cannabis plants attach. These novel psychoactive substances should not be confused with syntheti ...
References
{{Cannabinoids
Adamantanes
Cannabinoids
Designer drugs
Indazolecarboxamides